货号:A463156 同义名: PRT054021;MK-4448
Betrixaban is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM (inhibition of Factor 10a).
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产品名称 | Factor Xa ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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Rivaroxaban |
++
Factor Xa, IC50: 0.7 nM |
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Apixaban |
++++
Factor Xa (human), Ki: 0.08 nM Factor Xa (rabbit), Ki: 0.17 nM |
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Edoxaban tosylate monohydrate |
+++
Factor Xa, Ki: 0.561 nM |
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Serine protease factor Xa (fXa), positioned at the juncture of the intrinsic and the extrinsic pathways, play a pivotal role in the blood coagulation cascade [3]. Betrixaban is a highly potent, selective, and orally efficacious fXa inhibitor with IC50of 1.5 nM. In patch clamp hERG (human ether-a-go-go related gene) assays, Betrixaban has IC50 value of 8.9 μM. The plasma kallikrein IC50 and Ki values for Betrixaban are 6.3 μM and 3.5 μM respectively. Betrixaban (hERG Ki 1.8 μM) exhibits significantly lower hERG activity than all the others (hERG Ki⩽0.5 μM) [3]. Dosed at 0.5 mg/kg IV and 2.5 mg/kg PO, Betrixaban has bioavailability of 51.6% in dog; dosed at 0.75 mg/kg IV and 7.5 mg/kg PO, Betrixaban has bioavailability of 58.7% in monkey [3]. After i.v. infusion for 30 min, the total plasma concentration of Betrixaban is 0.2±0.01 μM, and the percentage of unbound inhibitor is 40%±7.2% [4]. |
作用机制 | The chloropyridine A ring extents into the fXa S1 site with the chloro atom positioned above the phenyl ring of Tyr228 and occupies a hydrophobic pocket formed by Ala190, Val213 and Tyr228. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03728166 | Venous Thromboembolism | Phase 4 | Not yet recruiting | February 1, 2021 | - |
NCT03397888 | Hepatic Impairment | Phase 1 | Completed | - | United States, Florida ... 展开 >> Clinical Pharmacology of Miami Hialeah, Florida, United States, 33014 收起 << |
NCT03613402 | - | Suspended(Due to slow enrollme... 展开 >>nt.) 收起 << | January 2020 | United States, North Carolina ... 展开 >> Durham Durham, North Carolina, United States, 27705 收起 << | |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.21mL 0.44mL 0.22mL |
11.06mL 2.21mL 1.11mL |
22.13mL 4.43mL 2.21mL |
CAS号 | 330942-05-7 |
分子式 | C23H22ClN5O3 |
分子量 | 451.906 |
别名 | PRT054021;MK-4448;MLN1021 |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 25 mg/mL(55.32 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |